TAK-441CAS号: 1186231-83-3分子式: C28H31F3N4O6分子量: 576.56描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
TAK-441 is an orally active inhibitor of Hedgehog signaling(IC50 = 4.4 nM) with potent antitumor activity. TAK-441 suppresses transcription factor Gli1 mRNA expression and tumor growth.
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
可溶性/溶解性 |
DMSO:Soluble,H2O:Insoluble
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生物活性 | |
In vitro(体外研究) |
TAK-441 (0.03 nM–1 μM) inhibits Gli1 mRNA in the tumor and skin with IC50s of 45.7 and 113 μg/ml, respectively[3]. In LNCaP cells, TAK-441 (0.5-500 nM) delays the castration-resistant progression without affecting androgen withdrawal-induced Shh up-regulation or cell viability[4].
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In vivo(体内研究) |
In ptc1+/-p53-/- mice, oral administration of TAK-441 (1-25 mg/kg) shows strong and dose-dependent antitumor activity. In BALB/c-nu/nu mice, oral administration of TAK-441 (10-100 mg/kg) shows favorable exposure and good oral JPorption[4].
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